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Bis‐Tetrahydrofuran: a Privileged Ligand for Darunavir and a New Generation of HIV Protease Inhibitors That Combat Drug Resistance
Author(s) -
Ghosh Arun K.,
Ramu Sridhar Perali,
Kumaragurubaran Nagaswamy,
Koh Yasuhiro,
Weber Irene T.,
Mitsuya Hiroaki
Publication year - 2006
Publication title -
chemmedchem
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.817
H-Index - 100
eISSN - 1860-7187
pISSN - 1860-7179
DOI - 10.1002/cmdc.200600103
Subject(s) - darunavir , protease , potency , ligand (biochemistry) , hiv 1 protease , chemistry , drug resistance , human immunodeficiency virus (hiv) , drug , stereochemistry , combinatorial chemistry , pharmacology , virology , in vitro , biochemistry , biology , microbiology and biotechnology , enzyme , antiretroviral therapy , receptor , viral load
Two inhibitors that incorporate bis‐THF as an effective high‐affinity P 2 ligand for the HIV‐1 protease substrate binding site maintain impressive potency against mutant strains resistant to currently approved protease inhibitors. Crystallographic structures of protein–ligand complexes help to explain the superior antiviral property of these inhibitors and their potency against a wide spectrum of HIV‐1 strains.